Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T99799 | ||||
Target Name | Cholinesterase (BCHE) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Drug Info | IC50 = 236 nM | [12] | ||
(-)-DEBROMOFLUSTRAMINE B | Drug Info | IC50 = 1370 nM | [22] | ||
(-)-Phenethylcymserine | Drug Info | IC50 = 6 nM | |||
(-)-Phenserine | Drug Info | IC50 = 1560 nM | |||
(-)-Tolserine | Drug Info | IC50 = 1950 nM | |||
(1'H-Phenothiazin-1'-yl)(piperidin-1-yl)methanone | Drug Info | Ki = 1560 nM | [34] | ||
(10H-phenothiazin-10-yl)(m-tolyl)methanone | Drug Info | Ki = 1900 nM | [16] | ||
(10H-phenothiazin-10-yl)(o-tolyl)methanone | Drug Info | Ki = 3100 nM | [16] | ||
(10H-phenothiazin-10-yl)(p-tolyl)methanone | Drug Info | Ki = 2500 nM | [16] | ||
(10H-phenothiazin-10-yl)(phenyl)methanone | Drug Info | Ki = 5800 nM | [16] | ||
(24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol | Drug Info | Ki = 4600 nM | [4] | ||
(3-bromophenyl)(10H-phenothiazin-10-yl)methanone | Drug Info | Ki = 600 nM | [16] | ||
(4-bromophenyl)(10H-phenothiazin-10-yl)methanone | Drug Info | Ki = 1300 nM | [16] | ||
(4-nitrophenyl)(10H-phenothiazin-10-yl)methanone | Drug Info | Ki = 820 nM | [16] | ||
(RS)-tacrine(10)-hupyridone | Drug Info | IC50 = 81.5 nM | [20] | ||
1,10-bis(pyridinium)-decane dibromide | Drug Info | IC50 = 5000 nM | [33] | ||
1,11-bis(pyridinium)-undecane dibromide | Drug Info | IC50 = 7000 nM | [33] | ||
1,2-bis(2,3-fluorophenyl)ethane-1,2-dione | Drug Info | Ki = 1270 nM | [15] | ||
1,2-di(10H-phenothiazin-10-yl)ethane-1,2-dione | Drug Info | Ki = 220 nM | [16] | ||
1,2-Di(berberine-9-O-yl)ethane dibromide | Drug Info | IC50 = 1110 nM | [36] | ||
1,2-indanedione | Drug Info | Ki = 2630 nM | [18] | ||
1,2-NAPHTHOQUINONE | Drug Info | Ki = 2290 nM | [18] | ||
1,3-Di(berberine-9-O-yl)ethane dibromide | Drug Info | IC50 = 531 nM | [36] | ||
1,4-Di(berberine-9-O-yl)ethane dibromide | Drug Info | IC50 = 231 nM | [36] | ||
1,9-bis(pyridinium)-nonane dibromide | Drug Info | IC50 = 6000 nM | [33] | ||
1-(10H-phenothiazin-10-yl)-2-phenylbutan-1-one | Drug Info | Ki = 400 nM | [16] | ||
1-(10H-phenothiazin-10-yl)-2-phenylethanone | Drug Info | Ki = 610 nM | [16] | ||
1-(10H-phenothiazin-10-yl)-2-phenylpropan-1-one | Drug Info | Ki = 560 nM | [16] | ||
1-(10H-phenothiazin-10-yl)-3-phenylbutan-1-one | Drug Info | Ki = 1700 nM | [16] | ||
1-(10H-phenothiazin-10-yl)-3-phenylpropan-1-one | Drug Info | Ki = 6200 nM | [16] | ||
1-(10H-phenothiazin-10-yl)-4-phenylbutan-1-one | Drug Info | Ki = 220 nM | [16] | ||
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione | Drug Info | Ki = 12600 nM | [14] | ||
1-methyl-3-(phenylcarbamoyloxy)pyridinium bromide | Drug Info | IC50 = 550 nM | |||
2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine | Drug Info | IC50 = 7200 nM | [8] | ||
2-biphenyl-4-yl-1-phenothiazin-10-yl-ethanone | Drug Info | Ki = 1700 nM | [16] | ||
2-methoxyphenyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 340 nM | [21] | ||
2-Methyl-beta-carboline-2-ium iodide | Drug Info | IC50 = 540 nM | [35] | ||
2-Propyl-beta-carboline-2-ium iodide | Drug Info | IC50 = 2305 nM | [35] | ||
24-ethyl-cholest-7-ene-3,5,6-triol | Drug Info | Ki = 2500 nM | [4] | ||
24-ethylcholest-6-ene-3,5-diol | Drug Info | Ki = 4200 nM | [4] | ||
3,4,5,6-Tetrachloro-[1,2]benzoquinone | Drug Info | Ki = 3200 nM | [3] | ||
3-(2-Diethylamino-acetamino)-rutaecarpine | Drug Info | IC50 = 17620 nM | [30] | ||
3-(2-Diethylamino-propionamino)-rutaecarpine | Drug Info | IC50 = 2848 nM | [30] | ||
3-(2-N-Piperidyl-propionamino)-rutaecarpine | Drug Info | IC50 = 2112 nM | [30] | ||
3-(2-N-Pyrrolyl-acetamino)-rutaecarpine | Drug Info | IC50 = 696.1 nM | [30] | ||
3-(2-N-Pyrrolyl-propionamino)-rutaecarpine | Drug Info | IC50 = 844.5 nM | [30] | ||
3-(dimethylamino)phenyl phenylcarbamate | Drug Info | IC50 = 18000 nM | |||
3-chlorophenyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 570 nM | [21] | ||
3-isopr-sal-cyclosal-d4TMP | Drug Info | IC50 = 4700 nM | [13] | ||
3-methoxyphenyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 710 nM | [21] | ||
3-phenyl-cyclosal-d4TMP | Drug Info | IC50 = 350 nM | [13] | ||
3-sal-cyclosal-d4TMP | Drug Info | IC50 = 2300 nM | [13] | ||
3-[10-(benzylmethylamino)decyloxy]xanthen-9-one | Drug Info | IC50 = 100 nM | [10] | ||
3-[11-(benzylmethylamino)undecyloxy]xanthen-9-one | Drug Info | IC50 = 120 nM | [10] | ||
3-[12-(benzylmethylamino)dodecyloxy]xanthen-9-one | Drug Info | IC50 = 150 nM | [10] | ||
3-[3-(benzylmethylamino)propoxy]xanthen-9-one | Drug Info | IC50 = 8330 nM | [10] | ||
3-[4-(benzylmethylamino)butoxy]xanthen-9-one | Drug Info | IC50 = 2650 nM | [10] | ||
3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one | Drug Info | IC50 = 2490 nM | [10] | ||
3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one | Drug Info | IC50 = 1430 nM | [10] | ||
3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one | Drug Info | IC50 = 800 nM | [10] | ||
3-[8-(benzylmethylamino)octyloxy]xanthen-9-one | Drug Info | IC50 = 80 nM | [10] | ||
3-[9-(benzylmethylamino)nonyloxy]xanthen-9-one | Drug Info | IC50 = 100 nM | [10] | ||
4-chlorophenyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 10500 nM | [21] | ||
4-ISOPROPYLPHENSERINE | Drug Info | IC50 = 240 nM | [32] | ||
4-methoxyphenyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 2260 nM | [21] | ||
4-[4-(benzyloxy)piperidino]butyl benzoate | Drug Info | IC50 = 1890 nM | [17] | ||
4-[4-(benzyloxy)piperidino]butyl-3-chlorobenzoate | Drug Info | IC50 = 1350 nM | [17] | ||
4-[4-(benzyloxy)piperidino]butyl-3-fluorobenzoate | Drug Info | IC50 = 1580 nM | [17] | ||
4-[4-(benzyloxy)piperidino]butyl-4-chlorobenzoate | Drug Info | IC50 = 3520 nM | [17] | ||
4-[4-(benzyloxy)piperidino]butyl-4-fluorobenzoate | Drug Info | IC50 = 560 nM | [17] | ||
4-[4-(benzyloxy)piperidino]butyl-4-nitrobenzoate | Drug Info | IC50 = 5230 nM | [17] | ||
5,6-dinitroacenaphthoquinone | Drug Info | Ki = 3100 nM | [18] | ||
5-methyl-cyclosal-d4TMP | Drug Info | IC50 = 4600 nM | [13] | ||
6-chlorotacrine hydrochloride | Drug Info | IC50 = 916 nM | [26] | ||
6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium | Drug Info | IC50 = 2700 nM | [9] | ||
6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium | Drug Info | IC50 = 1600 nM | [9] | ||
6-hydroxy-2-methyl-9H-beta-carbolin-2-ium | Drug Info | IC50 = 8700 nM | [9] | ||
6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium | Drug Info | IC50 = 1200 nM | [9] | ||
6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indole | Drug Info | IC50 = 17400 nM | [9] | ||
6-methoxy-2-methyl-9H-beta-carbolin-2-ium | Drug Info | IC50 = 17500 nM | [9] | ||
7-Oxo-7H-dibenzo[de,g]quinoline | Drug Info | IC50 = 4010 nM | [25] | ||
9-Ethyl-2-methyl-beta-carboline-2-ium iodide | Drug Info | IC50 = 2019 nM | [35] | ||
9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide | Drug Info | IC50 = 3000 nM | [28] | ||
9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide | Drug Info | IC50 = 4180 nM | [28] | ||
9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide | Drug Info | IC50 = 4160 nM | [36] | ||
9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromide | Drug Info | IC50 = 5440 nM | [36] | ||
9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide | Drug Info | IC50 = 2050 nM | [36] | ||
9-O-[3-(Phenylamino)propyl]-berberine bromide | Drug Info | IC50 = 1760 nM | [36] | ||
9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromide | Drug Info | IC50 = 2220 nM | [28] | ||
9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide | Drug Info | Ki = 1020 nM | [28] | ||
9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide | Drug Info | IC50 = 2690 nM | [28] | ||
ACENAPHTHOQUINONE | Drug Info | Ki = 2970 nM | [18] | ||
Anthracen-10-yl(10H-phenothiazin-10-yl)methanone | Drug Info | Ki = 3.5 nM | [16] | ||
AS-1397 | Drug Info | IC50 = 3370 nM | [11] | ||
BENZOQUINONE | Drug Info | Ki = 2050 nM | [3] | ||
Bis-7-tacrine | Drug Info | IC50 = 10.5 nM | [37] | ||
Bis-cyclosal-d4TMP | Drug Info | IC50 = 14000 nM | [13] | ||
Butyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 13400 nM | [21] | ||
CAPROCTAMINE | Drug Info | IC50 = 11600 nM | [24] | ||
CHF-2819 | Drug Info | IC50 = 1700 nM | [2] | ||
CHLORANIL | Drug Info | Ki = 268 nM | [3] | ||
Cyclopentyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 3190 nM | [21] | ||
Cyclosal-d4TMP | Drug Info | IC50 = 770 nM | [13] | ||
DEMETHYLDEBROMOFLUSTRAMINE B | Drug Info | IC50 = 260 nM | [22] | ||
Eptastigmine | Drug Info | IC50 = 5 nM | [6] | ||
HALOXYSTEROL A | Drug Info | Ki = 4500 nM | [4] | ||
HALOXYSTEROL B | Drug Info | Ki = 2500 nM | [4] | ||
Haloxysterol C | Drug Info | Ki = 18000 nM | [4] | ||
Haloxysterol D | Drug Info | Ki = 2200 nM | [4] | ||
Huprine X | Drug Info | Ki = 120 nM | [7] | ||
Iso-OMPA | Drug Info | IC50 = 733 nM | [23] | ||
Isopropyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 18100 nM | [21] | ||
Isosorbide-2-(benzylcarbamate)-5-benzoate | Drug Info | IC50 = 4.3 nM | [23] | ||
Isosorbide-2-(benzylcarbamate)-5-mononitrate | Drug Info | IC50 = 3.6 nM | [23] | ||
Isosorbide-2-(butylcarbamate)-5-benzoate | Drug Info | IC50 = 72 nM | [23] | ||
Isosorbide-2-(butylcarbamate)-5-mononitrate | Drug Info | IC50 = 894 nM | [23] | ||
Isosorbide-2-(cyclohexylcarbamate)-5-mononitrate | Drug Info | IC50 = 2500 nM | [23] | ||
Isosorbide-2-(ethylcarbamate)-5-mononitrate | Drug Info | IC50 = 3900 nM | [23] | ||
Isosorbide-2-(methylcarbamate)-5-benzoate | Drug Info | IC50 = 669 nM | [23] | ||
Isosorbide-2-(methylcarbamate)-5-mononitrate | Drug Info | IC50 = 5100 nM | [23] | ||
Isosorbide-2-(propylcarbamate)-5-mononitrate | Drug Info | IC50 = 639 nM | [23] | ||
Isosorbide-2-benzyl carbamate | Drug Info | IC50 = 3700 nM | [29] | ||
Isosorbide-2-benzylcarbamate-5-(o-toluate) | Drug Info | IC50 = 1.2 nM | [29] | ||
Isosorbide-2-benzylcarbamate-5-acetate | Drug Info | IC50 = 4100 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-cyclopentanoate | Drug Info | IC50 = 6 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-cyclopropanoate | Drug Info | IC50 = 334 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-isonicotinate | Drug Info | IC50 = 88 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-nicotinate | Drug Info | IC50 = 57 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-pentanoate | Drug Info | IC50 = 700 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-propionate | Drug Info | IC50 = 980 nM | [23] | ||
Isosorbide-2-benzylcarbamate-5-triflate | Drug Info | IC50 = 359 nM | [23] | ||
Isosorbide-di-(benzylcarbamate) | Drug Info | IC50 = 400 nM | [31] | ||
Isosorbide-di-(butylcarbamate) | Drug Info | IC50 = 1220 nM | [31] | ||
Isosorbide-di-(propylcarbamate) | Drug Info | IC50 = 10400 nM | [31] | ||
LAWSARITOL | Drug Info | Ki = 3700 nM | [4] | ||
LIPOCRINE | Drug Info | IC50 = 11 nM | [27] | ||
M-tolyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 1690 nM | [21] | ||
MEMOQUIN | Drug Info | IC50 = 1440 nM | [27] | ||
MEPTAZINOL | Drug Info | IC50 = 15000 nM | [19] | ||
Methyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 10200 nM | [21] | ||
Morpholino(1'H-phenothiazin-1'-yl)methanone | Drug Info | Ki = 7100 nM | [34] | ||
N,N'-(1',10'-decylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 17 nM | [19] | ||
N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP | Drug Info | IC50 = 74 nM | [19] | ||
N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP | Drug Info | IC50 = 100 nM | [19] | ||
N,N'-(1',2'-ethylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 125 nM | [19] | ||
N,N'-(1',3'-propylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 132 nM | [19] | ||
N,N'-(1',4'-butylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 104 nM | [19] | ||
N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 192 nM | [19] | ||
N,N'-(1',6-hexylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 119 nM | [19] | ||
N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 102 nM | [19] | ||
N,N'-(1',8'-octylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 63 nM | [19] | ||
N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP | Drug Info | IC50 = 10 nM | [19] | ||
N,N-Diethyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 1050 nM | [34] | ||
N,N-Diisopropyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 180 nM | [34] | ||
N,N-Dimethyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 9200 nM | [34] | ||
N,N-Dipropyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 430 nM | [34] | ||
N-(Adamant-1-yl)-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 350 nM | [34] | ||
N-Benzyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 4450 nM | [34] | ||
N-benzyl-2-thiomorpholinopyrimidin-4-amine | Drug Info | IC50 = 2300 nM | [37] | ||
N-Cyclobutyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 10000 nM | [34] | ||
N-Cyclohexyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 2810 nM | [34] | ||
N-Cyclopentyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 2990 nM | [34] | ||
N-Isopropyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 3410 nM | [34] | ||
N-Methyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 18300 nM | [34] | ||
N-n-heptyl-7-methoxytacrine hydrochloride | Drug Info | IC50 = 40 nM | [38] | ||
N-n-hexyl-7-methoxytacrine hydrochloride | Drug Info | IC50 = 1000 nM | [38] | ||
N-n-nonyl-7-methoxytacrine hydrochloride | Drug Info | IC50 = 360 nM | [38] | ||
N-n-octyl-7-methoxytacrine hydrochloride | Drug Info | IC50 = 120 nM | [38] | ||
N-n-pentyl-7-methoxytacrine hydrochloride | Drug Info | IC50 = 16000 nM | [38] | ||
N-Neopentyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 2660 nM | [34] | ||
N-o-Tolyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 710 nM | [34] | ||
N-p-Tolyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 12100 nM | [34] | ||
N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine | Drug Info | IC50 = 13800 nM | [37] | ||
N-Phenyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 310 nM | [34] | ||
N-tert-Butyl-1'H-phenothiazine-1'-carboxamide | Drug Info | Ki = 10600 nM | [34] | ||
Naphthalen-1-yl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 36 nM | [21] | ||
Naphthalen-1-yl(10H-phenothiazin-10-yl)methanone | Drug Info | Ki = 88 nM | [16] | ||
Naphthalen-2-yl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 120 nM | [21] | ||
Naphthalen-2-yl(10H-phenothiazin-10-yl)methanone | Drug Info | Ki = 470 nM | [16] | ||
NOSTOCARBOLINE | Drug Info | IC50 = 13200 nM | [5] | ||
NSC-23180 | Drug Info | Ki = 1670 nM | [18] | ||
O-tolyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 390 nM | [21] | ||
P-tolyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 2850 nM | [21] | ||
Phenanthrene-9,10-dione | Drug Info | Ki = 190 nM | [18] | ||
Phenyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 570 nM | [21] | ||
Tert-butyl 10H-phenothiazine-10-carboxylate | Drug Info | Ki = 4300 nM | [21] | ||
TOLSERINE | Drug Info | IC50 = 1950 nM | [6] | ||
VAGANINE D | Drug Info | IC50 = 10000 nM | [1] | ||
XANTHOSTIGMINE | Drug Info | IC50 = 48 nM | [39] | ||
References | |||||
REF 1 | Steroidal alkaloids from the leaves of Sarcococca coriacea of Nepalese origin. J Nat Prod. 2001 Jun;64(6):842-4. | ||||
REF 2 | Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine. J Med Chem. 2005 Feb 24;48(4):986-94. | ||||
REF 3 | Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. J Med Chem. 2005 Apr 21;48(8):2906-15. | ||||
REF 4 | Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum. Bioorg Med Chem Lett. 2006 Feb;16(3):573-80. | ||||
REF 5 | Nostocarboline: isolation and synthesis of a new cholinesterase inhibitor from Nostoc 78-12A. J Nat Prod. 2005 Dec;68(12):1793-5. | ||||
REF 6 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. J Med Chem. 2006 Apr 6;49(7):2174-85. | ||||
REF 7 | Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites. J Med Chem. 2006 Jun 1;49(11):3421-5. | ||||
REF 8 | Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase. J Med Chem. 2006 Sep 7;49(18):5411-3. | ||||
REF 9 | 6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5840-3. | ||||
REF 10 | Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones. Bioorg Med Chem. 2007 Jan 1;15(1):575-85. | ||||
REF 11 | Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. J Med Chem. 2006 Dec 14;49(25):7540-4. | ||||
REF 12 | Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the ox... J Med Chem. 2006 Nov 16;49(23):6833-40. | ||||
REF 13 | Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides. J Med Chem. 2007 Mar 22;50(6):1335-46. | ||||
REF 14 | Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. J Med Chem. 2007 Apr 19;50(8):1876-85. | ||||
REF 15 | Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils. Bioorg Med Chem. 2007 Jun 1;15(11):3801-17. | ||||
REF 16 | Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine. Bioorg Med Chem. 2007 Oct 1;15(19):6367-78. | ||||
REF 17 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abe... Bioorg Med Chem. 2007 Oct 15;15(20):6596-607. | ||||
REF 18 | Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. J Med Chem. 2007 Nov 15;50(23):5727-34. | ||||
REF 19 | Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation. J Med Chem. 2008 Apr 10;51(7):2027-36. | ||||
REF 20 | Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely... J Med Chem. 2008 Jun 12;51(11):3154-70. | ||||
REF 21 | Carbamates with differential mechanism of inhibition toward acetylcholinesterase and butyrylcholinesterase. J Med Chem. 2008 Jul 24;51(14):4200-12. | ||||
REF 22 | Synthesis and biological evaluation of (-)- and (+)-debromoflustramine B and its analogues as selective butyrylcholinesterase inhibitors. J Med Chem. 2008 Sep 11;51(17):5271-84. | ||||
REF 23 | Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors. J Med Chem. 2008 Oct 23;51(20):6400-9. | ||||
REF 24 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inne... J Med Chem. 2008 Nov 27;51(22):7308-12. | ||||
REF 25 | Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinester... Eur J Med Chem. 2009 Jun;44(6):2523-32. | ||||
REF 26 | Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds. J Med Chem. 2009 Sep 10;52(17):5365-79. | ||||
REF 27 | Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks. J Med Chem. 2009 Dec 10;52(23):7883-6. | ||||
REF 28 | Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors. Bioorg Med Chem. 2010 Feb;18(3):1244-51. | ||||
REF 29 | Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor. J Med Chem. 2010 Feb 11;53(3):1190-9. | ||||
REF 30 | Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors. Eur J Med Chem. 2010 Apr;45(4):1415-23. | ||||
REF 31 | Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability. Bioorg Med Chem. 2010 Feb;18(3):1045-53. | ||||
REF 32 | Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1718-20. | ||||
REF 33 | Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for My... Bioorg Med Chem Lett. 2010 Mar 1;20(5):1763-6. | ||||
REF 34 | Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants. Bioorg Med Chem. 2010 Mar 15;18(6):2232-2244. | ||||
REF 35 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. J Med Chem. 2010 May 13;53(9):3611-7. | ||||
REF 36 | Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem. 2010 Jun 15;18(12):4475-84. | ||||
REF 37 | Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3606-9. | ||||
REF 38 | Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6093-5. | ||||
REF 39 | Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkox... J Med Chem. 1998 Oct 8;41(21):3976-86. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.